JPH059406B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to new cosmetic compositions that resist skin aging. The invention particularly relates to cosmetic compositions containing as active ingredient an extract of the fruit of Silybum Marianum. Siribum marianum L. (Gaertn.) or Carduus Marianum L.
The fruit extract contains Silybin, Silydianin, Silandrin, Silychristin, which is obtained by polymerization of Silybine.
Silymonin is a flavonolignan-rich mixture containing Silybinomer among others. The components mentioned above are stabilized in the extract by various polyphenols such as taxiphorol and other components such as dehydrodiconiferous alcohol. Siribum marianum fruit extract is
Wagner et al. “Arzneim Forsch” 1:8688,
It can be obtained by extraction from delipidated fruit with a solvent such as methanol, ethanol or acetone as described in J.D. 1968. Lipid removal can be obtained by using non-polar solvents such as carbon tetrachloride or petroleum ether. The above-mentioned plants and their active components are known for their liver-protecting activity and have traditionally been used in medicine for this purpose. The present inventor has discovered that the extract of Siribum marianum fruit has radical (free radical) inhibiting activity;
and siribum marianum fruit extract 0.01
It has been found that topical compositions containing ~1% by weight, especially 0.1-0.5% by weight, are able to resist the degrading effects of free radicals, which are partly related to skin aging. Free radicals are normally produced in very small amounts during the lifetime of a cell. They may be produced by the action of radiation in the ultraviolet and visible light spectra. The skin is particularly affected by the aforementioned production methods since it is directly exposed. However, free radicals are generated especially in physiological oxidation-reduction reactions. The radicals thus generated are usually removed by enzyme systems capable of destroying them. However, if the enzymatic system is too taxed, as a result of excessive radical production or incomplete detoxification mechanisms, the radicals will react with cellular components and degrade them. The cellular components that are the preferential targets of free radicals are of great functional importance. These components are primarily polyunsaturated fatty acids that form part of the composition of the phospholipids that form cell membranes. When radicals attack fatty acids, tissue destruction spreads throughout the membrane, interfering with its function, especially its role as a barrier within the epidermis, which ensures the correct hydration of the skin. Proteins such as enzyme proteins and structural proteins such as collagen and elastin, which are essential components of the epithelium, are also targets of free radicals. Finally, nucleic acids such as DNA (the carrier of the genetic code) are particularly susceptible to the degenerative effects of free radicals. Their deterioration, even minimal, continues over many years, resulting in irreversible biochemical damage that is partly related to cellular aging. Siribum marianum fruit extract can slow down the rate of skin aging due to its radical inhibiting activity. Therefore, the present invention uses the extract of Siribum marianum fruit as an active ingredient at a dry extract concentration of 0.01 to 0.01.
1% by weight, preferably from 0.1 to 0.5% by weight, for cosmetic compositions that resist skin aging. The inventor has also found that by adding 0.01 to 0.5% by weight of α-tocopherol to the composition, the effect on skin aging can be increased. It should be noted that α-tocopherol is already present in the extract of Siribum marianum fruit, but at low concentrations. Below, research on the radical inhibiting activity of the active ingredient used in the present invention will be shown. The composition used in the following studies was a solution in polyethylene glycol 400 (dry extract content 50 g/) of the ethanolic extract of Siribum marianum fruit, which had been delipidized. This solution is hereinafter referred to as SM extract. (1) Radical suppression activity against superoxide radical anions The formation of superoxide radical anions (O ₂ ^- )
It is an important step in the production of other reactive species of oxygen and the subsequent production of organic groups. Superoxide radicals are produced by a number of redox reactions catalyzed by enzymes such as xanthine oxidase. The protective effect of the SM extract is demonstrated with respect to the superoxide anion generated by the enzyme system in vitro in the presence of cytochrome C (the conversion of which is measured spectrophotometrically at 550 nm). The results are shown in Table 1. The results show that SM extract suppresses the conversion of cytochrome C by scavenging superoxide anions.

[Table] (2) Inhibition of peroxidation of polyunsaturated fatty acids (Bonne et al.
(1985, Annals of Allergy, 54, 158-160) Platelets are a very useful model for the study of free radical production and the products that can scavenge it within the cellular environment. In fact, platelets are
It is especially rich in enzymes that cause peroxidation of unsaturated fatty acids. These reactions are initiated by radical production and can be easily measured by chromatographic separation of metabolites formed from 14C-labeled fatty acids such as arachidonic acid. The above is metabolized mainly into thromboxane B2
(TxB2), hydroxyheptadecatrienoic acid + malonyl dialdehyde (HHT + MDA), and hydroxy-12-eicosatetraenoic acid (12-
HETE). These precursors are unstable peroxides. SM extract has an SM extract concentration of 0.10
~0.25% (calculated as dry extract) suppresses the production of the above-mentioned metabolites by preventing peroxide free radical production within the cells themselves. The results are shown in Table 1.

【table】

[Table] (3) Malonyldialdehyde (MDA) in the skin
Inhibition of Production One of the signs of cellular aging in which free radicals can be attributed to the aging process is the accumulation of lipofusin in tissues. These pigments are
Schiff bases are obtained from the reaction of malonyl dialdehyde (MDA), produced by free radical decomposition of lipids, with primary amines. The protective effect regarding this process is shown in the following tests (Table). In that study, when diluted to 5% in a cosmetic excipient and applied to the skin of hairless mice, SM extract inhibited the formation of MDA in the skin induced by UV radiation. . Hairless mice weighing 25-30 g are divided into groups of 5 and treated as described in the table. The ultraviolet irradiation intensity at 300 nm is 0.3 J/cm ² . Irradiation is stopped after 9 hours and the dorsal skin is removed, weighed and homogenized in buffered saline solution. Centrifuge the homogenate and remove MDA from the supernatant.
is determined spectrophotometrically after reaction with thiobarbituric acid.

[Table] The cosmetic compositions of the invention can also contain, if appropriate, any known substances that have beneficial properties for the skin. These substances are, for example, collagen, elastin, hyaluronic acid, lipids combined with unsaturated fatty acids, humectants (softeners), vitamin-rich extracts, perfumes, preservatives, and colorants. The composition may further contain a sunlight exposure screen or filter. The cosmetic composition of the present invention can take any form used in cosmetics. for example,
Gels or creams in bottles or tubes, lotions or emulsions in glass or plastic bottles and, where appropriate, in dispensing bottles or ampoules. Therefore, the invention particularly relates to creams for the skin,
The present invention relates to cosmetic compositions in the form of gels, emulsions or lotions, and more particularly to cosmetic compositions in which excipients are adapted to be applied to the face or neck. Appropriate excipients are required for each specific cosmetic formulation. These excipients need to have all the required properties. for example,
Mention may be made of commonly used agents such as glycerol stearate, propylene glycol, lanolin, glycerol, cetyl alcohol, polyols, vegetable oils, animal oils, mineral oils, waxes, wetting agents, thickening agents, stabilizers and emulsifiers. The various forms of cosmetics described above are manufactured by methods used in the art. The invention also relates to a concentrate composition for preparing the cosmetic composition according to the invention, which comprises from 1 to 10% by weight (as dry extract) of the extract of the fruit of Siribum marianum and advantageously α- Tocopherol
0.2 to 2% by weight. This composition can be formulated into a suitable base for cosmetic compositions. As an example of such a concentrated composition, mention may be made of a polyethylene glycol solution of an alcoholic extract of Siribum marianum fruit from which lipids have been removed, such as the aforementioned SM extract containing 5% by weight of dry extract. Another example of such a composition is an SMT extract comprising 5% by weight of Siribum marianum fruit extract and 1% by weight of α-tocopherol in polyethylene glycol 400. Examples of cosmetic compositions are listed below (parts by weight). (1) O/W cream・Glycerol stearate 5・Mat oil 10・SM extract or SMT extract 2~10・Propylene glycol 3・Carboxyvinyl polymer 0.5・Triethanolamine 0.5・Aromatic composition Appropriate amount・Preservative Appropriate amount - Water to make 100 (2) O/W milk - Oleyl alcohol polyethoxy ether phosphate 2 - Cetyl alcohol 0.5 - Anhydrous lanolin 0.5 - Liquid silicone 1 - Malt oil 2 - Stearic acid 3 - Triethanolamine 0.5 - SM extract or SMT extract 2 to 6 ・ Magnesium aluminum silicate 0.5 ・ Aromatic composition appropriate amount ・ Preservative appropriate amount ・ Water appropriate amount (3) Aqueous-alcoholic lotion ・ Cetyl alcohol 0.5 ・ Stearic acid 5 ・ Glycerol 2 ・ SM Extract or SMT extract 3 - Sodium alginate 0.3 - Triethanolamine 0.5 - 94° alcohol 5 - Water 83.7 (4) Alcohol-based hydrogel - 40° alcohol 95 - Triethylamine 1.5 - EDTA 0.05 - SM extract or SMT extract 5・ Carbopol 940 1.5 (5) Glyceridated hydrogel ・ Sodium alginate 8 ・ Glycerol 25 ・ Borax (15%) in glycerol 20 ・ SM extract or SMT extract 5 ・ Thymol 2 ・ Water 45

Claims (1)

[Scope of Claims] 1. A cosmetic composition for preventing skin aging, which contains an extract of Siribum marianum fruit as an active ingredient at a dry extract concentration of 0.01 to 1% by weight. 2. A composition according to claim 1, containing from 0.1 to 0.5% by weight, calculated as dry extract, of the fruit extract of Siribum marianum. 3. The composition according to claim 1 or 2, which contains an alcoholic extract of Siribum marianum fruit as an active ingredient. 4. The composition according to claim 3, comprising a polyethylene glycol solution of an alcoholic extract of Siribum marianum fruit from which lipids have been removed. 5. The composition according to any one of claims 1 to 4, containing 0.1 to 0.2% by weight of α-tocopherol.